FB23-2 是一种有效、选择性的 mRNA N6- 甲基腺嘌呤脱甲基酶FTO抑制剂，IC50值为 2.6 μM。FB23-2 具有抗增殖作用。FB23-2 能用于急性髓系白血病 (AML) 的研究。
| 生物活性 | FB23-2 is a potent and selective inhibitor of mRNA N6-methyladenosine (m6A) demethylaseFTO, with anIC50of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML)[1]. |
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体外研究
(In Vitro) | FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human AML cell line cells and primary blast AML cells[1].
FB23 inhibits the proliferation of NB4 and MONOMAC6 cells, with IC50values of 0.8 μM and 1.5 μM[1].
FB23-2 (20 μM; 72 hours) displays anti-proliferation effect via upregulating global m6A levels[1].
FB23-2 (0.5-5 μM; 24-72 hours) significantly suppresses the proliferation of BM cells from these two models in a dose-dependent manner[1].
FB23-2 exhibits FTO-dependent anti-proliferation activity and promotes myeloid differentiation and apoptosis[1].
FB23-2 (1-20 μM; 72 hours) significantly increases the mRNA and protein levels of ASB2 and RARA in NB4 and MONOMAC6 cells[1].
FB23-2 induces apoptosis (1-20 μM; 48-72 hours) and cell cycle arrest (5-20 μM; 24 hours) at G1 stage in AML cells[1].
Cell Proliferation Assay[1] | Cell Line: | MA9 cells, FLT3ITD/NPM1 cells (mouse BM cells) | | Concentration: | 0.5 μM, 2 μM, 5 μM | | Incubation Time: | 24 hours, 48 hours, 72 hours | | Result: | Suppressed the proliferation of BM cells. |
RT-PCR[1] | Cell Line: | NB4 cells, MONOMAC6 cells | | Concentration: | 1 μM, 5 μM , 20 μM | | Incubation Time: | 72 hours | | Result: | Significantly increased ASB2 and RARA mRNA levels. |
Apoptosis Analysis[1] | Cell Line: | NB4 cells, MONOMAC6 cells | | Concentration: | 1 μM, 5 μM , 20 μM | | Incubation Time: | 48 hours (NB4 cells),72 hours (MONOMAC6 cells) | | Result: | Induced apoptosis. |
Cell Cycle Analysis[1] | Cell Line: | MONOMAC6 cells | | Concentration: | 5 μM , 20 μM | | Incubation Time: | 24 hours | | Result: | Induced cell cycle arrest at G1 stage. |
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体内研究
(In Vivo) | FB23-2 (2 mg/kg; i.p.; daily; for 10 days) substantially suppresses leukemia progression and prolongs survival[1].
FB23-2 exhibits elimination half-life (rat 6.7 h) and Cmax(rat 2421.3 ng/mL) following intraperitoneal injection (rat 3 mg/kg)[1].
| Animal Model: | NOD/LtSz-scid IL2RG-SGM3 (NSGS) mice, xeno-transplanted with MONOMAC6 AML cells[1] | | Dosage: | 2 mg/kg | | Administration: | Intraperitoneal injection, daily, for 10 days | | Result: | Delayed the onset of full-blown leukemic symptoms and significantly prolonged survival by almost doubling the median survival. |
| Animal Model: | Sprague Dawley (SD) rats[1] | | Dosage: | 3 mg/kg (Pharmacokinetic Analysis) | | Administration: | Intraperitoneal injection | | Result: | T1/2(6.7 hours), Cmax(2421.3 ng/mL). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(63.74 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5495 mL | 12.7473 mL | 25.4946 mL | | 5 mM | 0.5099 mL | 2.5495 mL | 5.0989 mL | | 10 mM | 0.2549 mL | 1.2747 mL | 2.5495 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 50%PEG300 50% saline Solubility: 10 mg/mL (25.49 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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